
3-Aminotetrahydrofurans form part of several pharmacologically active compounds. They seem to confer certain desirable properties on the investigational drug structures. A series of G-protein coupled adenosine receptors mediate cardiac and antilipolytic activities. In particular, selective adenosine A1 receptors have received attention for possible antiarrhythmic activity. For example, 3-(R)-aminotetrahydrofuranyl moiety formed an integrative structural feature of selective, high affinity adenosine A1 receptor agonists (Elzein, E; Kalla, R; Li, X; Perry, T; Marquart, T; Micklatcher, M; Li, Y; Wu, Y; Zeng, D and Zablocki, J, Bioorg. Med. Chem. Lett., 2007, 77, 161). 3-Aminotetrahydrofuranyl moiety also formed part of structural features of orally bioavailable experimental CGRP receptor antagonists (Bell, 1 M; Bednar, R A; Fay, J F; Gallicchio, S N; Hochman, J H; McMasters, D R; Miller-Stein, C; Moore, E L; Mosser, S D; Pudvah, N T; Quigley, A G; Salvatore, C A; Stump, C A; Theberge, C R; Wong B K; Zartman, C B; Zhang, X-F; Kane, S A; Graham, S L; Vacca, J P and Williams, T M, Bioorg. Med. Chem. Lett., 2006, 76, 6165). In spite of such extensive uses of 3-aminotetrahydrofuran in medicinal chemistry, methods to obtain chiral forms are scarce and hard to practice